1. PI3K/Akt/mTOR
    Anti-infection
  2. PI4K
    PI3K
    Virus Protease
  3. PIK-93

PIK-93 

Cat. No.: HY-12046 Purity: 99.37%
Handling Instructions

PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.

For research use only. We do not sell to patients.

PIK-93 Chemical Structure

PIK-93 Chemical Structure

CAS No. : 593960-11-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
5 mg USD 102 In-stock
Estimated Time of Arrival: December 31
10 mg USD 186 In-stock
Estimated Time of Arrival: December 31
50 mg USD 816 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.

IC50 & Target[1]

PI4KIIIβ

19 nM (IC50)

PI4KIIIα

1.1 μM (IC50)

p110γ

16 nM (IC50)

p110α

39 nM (IC50)

p110δ

120 nM (IC50)

p110β

590 nM (IC50)

PI3KC2β

140 nM (IC50)

PI3KC2α

16 μM (IC50)

hsVPS34

320 nM (IC50)

DNA-PK

64 nM (IC50)

ATM

490 nM (IC50)

mTORC1

1.38 μM (IC50)

ATR

17 μM (IC50)

In Vitro

PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 μM, and 0.12 μM, respectively. PIK-93 shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 μM[1]. In differentiated HL60 (dHL60) cells, PIK-93 (0.5 μM-1 μM) impairs consolidation and stability of the leading edge formed after treatment with uniform f-Met-Leu-Phe (fMLP). PIK-93 alters the localization, but not the amount, of the fMLP-dependent accumulation of total F-actin. In fMLP gradients, PIK-93 reduces the chemotactic index and triples the cells' turning frequency[2]. In COS-7 cells, PIK-93 (250 nM) effectively abrogates the accumulation of CERT-PH domain and FL-Cer in Golgi. PIK-93 of the same concentration also significantly inhibits the conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin. These facts indicate a key role of PI4KIIIβ in ceramide transport between the ER and Golgi, as well as in the regulation of spingomyelin synthesis[3]. In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry[4]. A recent report shows that PIK-93 has anti-enterovirus effects, as revealed by its inhibition of both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC50 values of 0.14 µM and 1.9 µM, respectively[5].

Molecular Weight

389.88

Formula

C₁₄H₁₆ClN₃O₄S₂

CAS No.

593960-11-3

SMILES

CC(NC1=NC(C)=C(S1)C2=CC=C(C(S(=O)(NCCO)=O)=C2)Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (384.73 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5649 mL 12.8245 mL 25.6489 mL
5 mM 0.5130 mL 2.5649 mL 5.1298 mL
10 mM 0.2565 mL 1.2824 mL 2.5649 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.55 mg/mL (11.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

IC50 values are measured using a standard TLC assay for lipid kinase activity. Kinase reactions are performed by preparing areaction mixture containing kinase, PIK-93 (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 µg/mL). Reactions are initiated by the addition of ATP containing 10 µCi of γ-32P-ATP to a final concentration 10 or 100 µM, and allowed to proceed for 20 min at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 µL 1N HCl followed by 160 µL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3 hours-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. Kinase activity is typically measured at 10-12 concentrations of PIK-93 representing two-fold dilutions from the highest concentration of 100 μM.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For actin staining, dHL60 cells are preincubated in suspension with PIK-93 or vehicle for 40 min, centrifuged for 5 min at 2000 rpm at room temperature in a J6-B centrifuge, resuspended in mHBSS containing the respective agent at the same concentration, allowed to stick to fibronectin-covered coverslips, and subjected to stimulation with a uniform concentration of 100 nM f-Met-Leu-Phe (fMLP) for 3 min. Cells are fixed in 3.7% PFA and stained with 10 units/mL rhodamine-phalloidin for 15 min.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.37%

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Keywords:

PIK-93PIK93PIK 93PI4KPI3KVirus ProteasePhosphatidylinositol 4 kinasesPI4 kinasesPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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PIK-93
Cat. No.:
HY-12046
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